目录号 | 产品详情 | 靶点 | |
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T10358L2 | Others | ||
Netarsudil mesylate is an inhibitor of Rho-associated protein kinase (ROCK) and norepinephrine transporter (NET) with effective in intraocular pressure (IOP) reduction. | |||
T16855 | ROCK | ||
SB-772077B dihydrochloride is an aminofurazan-based Rho kinase inhibitor (IC50s: 5.6 nM and 6 nM toward ROCK1 and ROCK2, respectively). | |||
T69123 | |||
NSC-2488 is a novel Rho-Kinase-II Inhibitor with Vasodilatory Activity. | |||
T28608 | |||
ROCKII-IN-DI is a potent, competitive inhibitor of Rho-associated coiled-coil-containing protein kinase 2 (ROCKII). | |||
T35828 | |||
Potent and selective Rho-kinase inhibitor (IC50 values are 3 and 56 nM for ROCK-II and ROCK-I respectively). Feng et al (2008) Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J.Med.Chem. 51 6642 PMID:18834107 | |||
T28469 | |||
PT-262 is a ROCK (Rho-associated coiled-coil forming protein kinase) inhibitor. It induces cytoskeleton remodeling and migration inhibition in lung carcinoma cells. | |||
T71120 | |||
AR-13503, is an metabolite of Netarsudil (AR-11324), is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and/or reducing intraocular pressure. | |||
T10357 | Others | ||
AR-13324 analog mesylate is an inhibitor of Rho-kinase and a norepinephrine transporter and reduces intraocular pressure in normotensive monkey eyes. | |||
T26821 | |||
BIPM is a potent inhibitor of Rho-associated protein kinase 2 (ROCK2). Exposure of SH-SY5Y cells to BIPM led to significant changes in cell migration, actin stress fibers and neurite length. BIPM significantly inhibits phosphorylation of cofilin, a regula | |||
T70108 | |||
Fasudil hydrochloride hydrate is an HCl salt of Fasudil -- a Rho-kinase (ROCK) inhibitor that has been shown to be effective in hindering the development of mature Cerebral Cavernous Malformation (CCM) lesions as well as reducing portal venous pressure in cirrhotic rats. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-01958 | RhoA Protein, Human, Recombinant (His) | Human | Baculovirus Insect Cells | ||
Transforming protein RhoA, also known as Rho cDNA clone 12, Ras homolog gene family member A, RHOA and ARH12, is a cell membrane and cytoplasm protein that belongs to the small GTPase superfamily and Rho family. The Rho family of small GTPases plays a key role in the dynamic regulation of the actin cytoskeleton that underlies various important cellular functions such as shape changes, migration, and polarity. RHOA / ARH12 is part of a larger family of related proteins known as the Ras superfamily; proteins involved in the regulation and timing of cell division. RHOA / ARH12 is a small GTPase protein known to regulate the actin cytoskeleton in the formation of stress fibers. It acts upon two known effector proteins: ROCK1 (Rho-associated, coiled-coil containing protein kinase 1) and DIAPH1 ( diaphanous homolog 1 (Drosophila) ). RHOA / ARH12 regulates a signal transduction pathway linking plasma membrane receptors to the assembly of focal adhesions and actin stress fibers. RHOA / ARH12 serves as a target for the yopT cysteine peptidase from Yersinia pestis, vector of the plague, and Yersinia pseudotuberculosis, which causes gastrointestinal disorders. RHOA / ARH12 may be an activator of PLCE1. It is activated by ARHGEF2, which promotes the exchange of GDP for GTP.
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TMPY-04397 | PAK-3 Protein, Human, Recombinant (His) | Human | Baculovirus Insect Cells | ||
PAK3 is a member of PAK proteins, a family of serine/threonine p21-activating kinases, serve as effectors of small Rho GTPases Cdc42 and RAC and have been implicated in a wide range of biological activities. There are six mammalian PAKs which can be divided into two groups: group I PAKs (PAK1-3) and group II PAKs (PAK4-6). Although the two PAK groups are architecturally similar there are differences in their mode of regulation suggesting their cellular functions are likely to be different. Group I p21-activated kinases (PAK1/2/3) is demonstrated as ERK3/ERK4 activation loop kinases. It has been shown that group I PAKs phosphorylate ERK3 and ERK4 on Ser-189 and Ser-186, respectively, both in vitro and in vivo, and that expression of activated Rac1 augments this response. Besides regulation enzymatic activation of ERK3/ERK4, PAKs can also play roles in downstream activation of MAP kinase-activated protein kinase 5 (MK5) in vivo. Thus, the group I PAKs act as upstream activators of ERK3 and ERK4 and unravel a novel PAK-ERK3/ERK4-MK5 signaling pathway. In clinical, PAK has been proposed as a potential therapeutic target in schwannomas.
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TMPH-03764 | YAP1 Protein, Human, Recombinant (His) | Human | P. pastoris (Yeast) | ||
Transcriptional regulator which can act both as a coactivator and a corepressor and is the critical downstream regulatory target in the Hippo signaling pathway that plays a pivotal role in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein STK3/MST2 and STK4/MST1, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1, which in turn phosphorylates and inactivates YAP1 oncoprotein and WWTR1/TAZ. Plays a key role in tissue tension and 3D tissue shape by regulating cortical actomyosin network formation. Acts via ARHGAP18, a Rho GTPase activating protein that suppresses F-actin polymerization. Plays a key role in controlling cell proliferation in response to cell contact. Phosphorylation of YAP1 by LATS1/2 inhibits its translocation into the nucleus to regulate cellular genes important for cell proliferation, cell death, and cell migration. The presence of TEAD transcription factors are required for it to stimulate gene expression, cell growth, anchorage-independent growth, and epithelial mesenchymal transition (EMT) induction. Suppresses ciliogenesis via acting as a transcriptional corepressor of the TEAD4 target genes AURKA and PLK1. In conjunction with WWTR1, involved in the regulation of TGFB1-dependent SMAD2 and SMAD3 nuclear accumulation.; Activates the C-terminal fragment (CTF) of ERBB4 (isoform 3).; Activates the C-terminal fragment (CTF) of ERBB4 (isoform 3).
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